Assay Detail
Functional
CHEMBL5144253
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Leishmanicidal activity against GFP-expressing axenic amastigote stage of Leishmania infantum MCAN/ES/89/IPZ229/1/89 infected in human THP-1 macrophage cells assessed as reduction in intracellular amastigotes incubated for 48 hrs by propidium iodide staining based flow cytometry
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Leishmania infantum |
| Cell Type | THP-1 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Pyridazino-pyrrolo-quinoxalinium salts as highly potent and selective leishmanicidal agents targeting trypanothione reductase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 5 | 5.77 | 6.26 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL125 | MILTEFOSINE | 4.0 | 1 | 6.26 |
| CHEMBL5170383 | — | — | 1 | 5.91 |
| CHEMBL5169813 | — | — | 1 | 5.75 |
| CHEMBL5189111 | — | — | 1 | 5.51 |
| CHEMBL5196304 | — | — | 1 | 5.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL125 | MILTEFOSINE | EC50 | = | 550.0 | nM | 6.26 |
| CHEMBL5170383 | — | EC50 | = | 1230.0 | nM | 5.91 |
| CHEMBL5169813 | — | EC50 | = | 1780.0 | nM | 5.75 |
| CHEMBL5189111 | — | EC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL5196304 | — | EC50 | = | 4020.0 | nM | 5.40 |